Synthesis, anticonvulsant activity, and neuropathic pain-attenuating activity of N-benzyl 2-amino-2-(hetero) aromatic acetamides

…, C Salomé, M De Ryck, R Kaminski, L Provins…

Index: Baruah, Pranjal K.; Dinsmore, Jason; King, Amber M.; Salome, Christophe; De Ryck, Marc; Kaminski, Rafal; Provins, Laurent; Kohn, Harold Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 11 p. 3551 - 3564

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Citation Number: 12

Abstract

N-Benzyl 2-acetamido-2-substituted acetamides, where the 2-substituent is a (hetero) aromatic moiety, are potent anticonvulsants. We report the synthesis and whole animal pharmacological evaluation of 16 analogues where the terminal 2-acetyl group was removed to give the corresponding primary amino acid derivatives (PAADs). Conversion to the PAAD structure led to a substantial drop in seizure protection in animal tests, ...